Yttrium-90 and indium-111 labelling, receptor binding and biodistribution of [DOTA0,d-Phe1,Tyr3]octreotide, a promising somatostatin analogue for radionuclide therapy |
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Authors: | Marion de Jong Willem H Bakker Eric P Krenning Wout A P Breeman Marcel E van der Pluijm Bert F Bernard Theo J Visser Eduard Jermann Martin Béhé Pia Powell Helmut R Mäcke |
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Affiliation: | (1) Department of Nuclear Medicine, University Hospital Dijkzigt, 3015 GD Rotterdam, The Netherlands;(2) Department of Internal Medicine III, University Hospital Dijkzigt, Rotterdam, The Netherlands;(3) Department of Nuclear Medicine, Kantonspital Basel, CH-4031 Basel, Switzerland |
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Abstract: | In vitro octreotide receptor binding of 111In-DOTA0,d-Phe1,Tyr3]octreotide (111In-DOTATOC) and the in vivo metabolism of90Y or111In-labelled DOTATOC were investigated in rats in comparison with 111In-DTPA0]octreotide 111In-DTPAOC).111In-DOTATOC was found to have an affinity similar to octreotide itself for the octreotide receptor in rat cerebral cortex microsomes. Twenty-four hours after injection of90Y or111In-labelled DOTATOC, uptake of radioactivity in the octreotide receptor-expressing tissues pancreas, pituitary, adrenals and tumour was a factor of 2–6 that after injection of111In-DTPAOC. Uptake of labelled DOTATOC in pituitary, pancreas, adrenals and tumour was almost completely blocked by pretreatment with 0.5 mg unlabelled octreotide, indicating specific binding to the octreotide receptors. These findings strongly indicate that90Y-DOTATOC is a promising radiopharmaceutical for radiotherapy and that111In-DOTATOC is of potential value for diagnosis of patients with octreotide receptor-positive lesions, such as most neuroendocrine tumours. |
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Keywords: | [DOTA0 d-Phe1" target="_blank">d-Phe1 Tyr3]octreotide Yttrium-90 Indium-111 Receptor binding Biodistribution |
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